Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7119-22. doi: 10.1016/j.bmcl.2012.09.077.

Casey McComas ¹, Jeffrey Cohen, Christine Huselton, Michael Marella, Edward Melenski, Cheryl Mugford, Ov Slayden, Richard Winneker, Jay Wrobel, Matthew R Yudt, Andrew Fensome

Affiliations

Affiliation

1 Chemical Sciences, Drug Safety and Metabolism, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19426, USA.

PMID: 23079530 DOI: 10.1016/j.bmcl.2012.09.077

Abstract

We have developed a new series of Progesterone Receptor modulators based upon the 4-aryl-phenylsulfonamide. Initial work in the series afforded potent compounds with good properties, however an advanced intermediate proved to be genotoxic in a non-GLP Ames assay following metabolic activation. We subsequently solved this problem and identified advanced leads which demonstrated oral efficacy in rhesus monkey pharmacodynamic and kinetics models.

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